Drug intelligence / Profile preview

tivantinib + gemcitabine

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Tivantinib (ARQ 197) is an orally available, selective, non–ATP-competitive small molecule inhibitor of the receptor tyrosine kinase c-MET (Hepatocyte growth factor receptor). c-MET is a key mediator of oncogenic signaling implicated in tumor cell migration, invasion, proliferation, and angiogenesis. Tivantinib has been investigated in combination with gemcitabine—a nucleoside analog and antimetabolite chemotherapy agent—for the treatment of various advanced solid tumors including pancreatic cancer. The combination aims to leverage tivantinib’s targeted inhibition of c-MET-driven pathways alongside the cytotoxic effects of gemcitabine on rapidly dividing tumor cells[1][2][6]. Tivantinib was developed by ArQule (now part of Merck KGaA), while gemcitabine is marketed under the brand name Gemzar by Eli Lilly.

Brand names
Gemzar
Other names
ARQ 197 plus gemcitabineARQ197 plus gemcitabineARQ-197 plus gemcitabinetivantinib plus gemcitabine
02

Targets

DNA polymerase familyTUBB (Tubulin (alpha and beta subunits))MET (Mesenchymal-epithelial transition factor receptor)

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